Design, characterization, and first-in-human study of the vascular actions of a novel biased apelin receptor agonist

[Pyr(1)]apelin-13 is an endogenous vasodilator and inotrope but is downregulated in pulmonary hypertension and heart failure, making the apelin receptor an attractive therapeutic target. Agonists acting at the same G-protein-coupled receptor can be engineered to stabilize different conformational st...

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Veröffentlicht in:	Hypertension (Dallas, Tex. 1979) Jg. 65; H. 4; S. 834
Hauptverfasser:	Brame, Aimee L, Maguire, Janet J, Yang, Peiran, Dyson, Alex, Torella, Rubben, Cheriyan, Joseph, Singer, Mervyn, Glen, Robert C, Wilkinson, Ian B, Davenport, Anthony P
Format:	Journal Article
Sprache:	Englisch
Veröffentlicht:	United States 01.04.2015
Schlagworte:	Animals Antipyretics Apelin Receptors Disease Models, Animal GTP-Binding Proteins - metabolism Humans Hypertension, Pulmonary - drug therapy Hypertension, Pulmonary - metabolism Hypertension, Pulmonary - physiopathology Intercellular Signaling Peptides and Proteins - pharmacology Male Rats Rats, Wistar Receptors, G-Protein-Coupled - agonists Receptors, G-Protein-Coupled - metabolism Research Design Saphenous Vein - drug effects Saphenous Vein - metabolism Saphenous Vein - physiopathology Vasodilation - drug effects pulmonary arterial hypertension [Pyr1]apelin-13 β-arrestin G-protein coupled receptors
ISSN:	1524-4563, 1524-4563
Online-Zugang:	Weitere Angaben
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